| Description: |
Esculin has neuroprotective, anti-oxidative, and anti-apoptotic effects, it is a plant coumarin compound that occur naturally in dietary plants or when supplemented in the diet probably inhibit the survival of E. coli O157 in the gut. Esculin has protective effects on dopamine(DA)-induced cytotoxicity in human neuroblastoma SH-SY5Y cells. Esculin has a protective effect on lipopolysaccharide (LPS)-induced acute lung injury (ALI) in mice, it can inhibit the Toll-like receptor-2 (TLR2), Toll-like receptor-4 (TLR4), myeloid differentiation primary response gene-88 (MyD88), and nuclear factor-κB (NF-κB) p65 in LPS-induced ALI. |
| Targets: |
TNF-α | TLR | NF-kB | ROS | p53 | Bcl-2/Bax | Caspase |
| In vitro: |
| Neuropharmacology. 2007 Nov;53(6):724-32 | | Anti-apoptotic effect of esculin on dopamine-induced cytotoxicity in the human neuroblastoma SH-SY5Y cell line.[Pubmed: 17904593 ] | Dopamine (DA), as a neurotoxin, can elicit severe Parkinson's disease-like syndrome by elevating intracellular reactive oxygen species (ROS) levels and apoptotic activity.
METHODS AND RESULTS:
In this study, we examined the effect of Esculin, which was extracted from Fraxinus sielboldiana blume, on DA-induced cytotoxicity and the underlying mechanism in human neuroblastoma SH-SY5Y cells. Our results suggest that the protective effects of Esculin (10(-7), 10(-6) and 10(-5) M) on DA-induced cytotoxicity may be ascribed to its anti-oxidative properties by reducing ROS level, and its anti-apoptotic effect via protecting mitochondrion membrane potential (DeltaPsim), enhancing superoxide dismutaese (SOD) activity and reduced glutathione (GSH) levels, and regulating P53, Bax and Bcl-2 expression. In addition, Esculin inhibited the release of cytochrome c and apoptosis-inducing factor (AIF), and the protein expression of activated caspase 3.
CONCLUSIONS:
These data indicate that Esculin may provide a useful therapeutic strategy for the treatment of progressive neurodegenerative diseases such as Parkinson's disease (PD). | | Plant Physiol . 2018 Oct;178(2):795-807. | | The Coumarin Glucoside, Esculin, Reveals Rapid Changes in Phloem-Transport Velocity in Response to Environmental Cues[Pubmed: 30111635] | | Abstract
The study of phloem transport and its vital roles in long-distance communication and carbon allocation have been hampered by a lack of suitable tools that allow high-throughput, real-time studies. Esculin, a fluorescent coumarin glucoside, is recognized by Suc transporters, including AtSUC2, which loads it into the phloem for translocation to sink tissues. These properties make it an ideal tool for use in live-imaging experiments, where it acts as a surrogate for Suc. Here, we show that Esculin is translocated with a similar efficiency to Suc and, because of its ease of application and detection, demonstrate that it is an ideal tool for in vivo studies of phloem transport. We used Esculin to determine the effect of different environmental cues on the velocity of phloem transport. We provide evidence that fluctuations in cotyledon Suc levels influence phloem velocity rapidly, supporting the pressure-flow model of phloem transport. Under acute changes in light levels, the phloem velocity mirrored changes in the expression of AtSUC2 This observation suggests that under certain environmental conditions, transcriptional regulation may affect the abundance of AtSUC2 and thus regulate the phloem transport velocity. |
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| In vivo: |
| Inflammation. 2015 Aug;38(4):1529-36. | | Esculin Inhibits the Inflammation of LPS-Induced Acute Lung Injury in Mice Via Regulation of TLR/NF-κB Pathways.[Pubmed: 25676436] |
METHODS AND RESULTS:
In this study, we investigated anti-inflammatory effects of Esculin (ESC) on lipopolysaccharide (LPS)-induced acute lung injury (ALI). ALI was induced in mice by intratracheal instillation of LPS, and ESC (20 and 40 mg/kg) was given orally 1 h prior to LPS administration. After 6 h, bronchoalveolar lavage fluid (BALF) and lung tissue were collected. ESC pretreatment decreased LPS-induced evident lung histopathological changes, lung wet-to-dry weight ratio, and lung myeloperoxidase activity. In addition, pretreatment with ESC inhibited inflammatory cells and proinflammatory cytokines including tumor necrosis factor-α (TNF-α), interleukin-1β, and interleukin-6 in BALF. Furthermore, we demonstrated that ESC inhibited the Toll-like receptor-2 (TLR2), Toll-like receptor-4 (TLR4), myeloid differentiation primary response gene-88 (MyD88), and nuclear factor-κB (NF-κB) p65 in LPS-induced ALI.
CONCLUSIONS:
The results indicated that the ESC had a protective effect on LPS-induced ALI in mice. | | Br J Nutr. 2004 May;91(5):749-55. | | Effects of esculin and esculetin on the survival of Escherichia coli O157 in human faecal slurries, continuous-flow simulations of the rumen and colon and in calves.[Pubmed: 15137927] | The human pathogen Escherichia coli O157:H7 is thought to be spread by direct or indirect contact with infected animal or human faeces.
METHODS AND RESULTS:
The present study investigated the effects of the plant coumarin Esculin and its aglycone esculetin on the survival of a strain of E. coli O157 under gut conditions. The addition of these compounds to human faecal slurries and in vitro continuous-flow fermenter models simulating conditions in the human colon and rumen caused marked decreases in the survival of an introduced strain of E. coli O157. When four calves were experimentally infected with E. coli O157 and fed Esculin, the pathogen was detected in five of twenty-eight (18 %) of faecal samples examined post-inoculation, compared with thirteen of thirty-five (37 %) of faecal samples examined from five control calves not fed Esculin.
CONCLUSIONS:
Coumarin compounds that occur naturally in dietary plants or when supplemented in the diet probably inhibit the survival of E. coli O157 in the gut. | | Mol Med Rep . 2018 May;17(5):7395-7402. | | Esculin ameliorates cognitive impairment in experimental diabetic nephropathy and induces anti-oxidative stress and anti-inflammatory effects via the MAPK pathway[Pubmed: 29568860] | | Abstract
Esculin is a derivative of coumarin, which is also an active ingredient of ash bark, and has antibacterial, anti-inflammatory, anti‑allergy and skin protective effects. The underlying mechanism and protective effects of Esculin on cognitive impairment in experimental diabetic nephropathy (DN) was investigated in the present study. Male C57BL/6J 6‑week‑old mice were injected intravenously with a single dose of streptozotocin (STZ; 30 mg/kg). At 2 weeks after the STZ injection, mice received intravenous injection with 5, 10 or 20 mg/kg Esculin for 2 weeks. In the present study, the results of the Morris water maze test demonstrated that Esculin significantly improved behavior and recognition memory in STZ‑induced diabetic rats. Furthermore, treatment of STZ‑induced diabetic rats with Esculin significantly inhibited tumor necrosis factor‑α, interleukin‑6, malondialdehyde, monocyte chemoattractant protein‑1 and intracellular adhesion molecule‑1 activity levels, and increased the activity of superoxide dismutase, in the kidney, which was determined by ELISA. In addition, Esculin treatment significantly suppressed the renal protein expression of activator protein 1, phosphorylated (p)‑p38 mitogen activated protein kinase (MAPK) and p‑c‑Jun N‑terminal kinase, and increased p‑extracellular signal regulated kinase 1/2 protein expression, in STZ‑induced diabetic rats, as determined by western blotting. These results indicate that Esculin may ameliorate cognitive impairment in experimental DN, and exert anti‑oxidative stress and anti‑inflammatory effects, via the MAPK signaling pathway. Thus, it may serve as a potential target for cognitive impairment of DN in the future. |
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